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    • 4. 发明申请
      US20120165337A1 TETRAHYDROQUINOXALINE UREA DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF 有权
    • TETRAHYDROQUINOXALINE UREA DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF
    • US20120165337A1
    • 2012-06-28
    • US13386830
    • 2010-07-23
    • Olivier Crespin , Eric Nicolai , Olivier Venier
    • Olivier Crespin , Eric Nicolai , Olivier Venier
    • A61K31/498 , A61P3/04 , A61P3/10 , A61P7/00 , A61P5/48 , A61P3/00 , A61P9/12 , A61P9/10 , A61P25/28 , A61P27/06 , A61P19/10 , A61P9/00 , A61P9/04 , A61P1/16 , A61P31/00 , A61P17/02 , C07D401/14
    • C07D401/12 , C07D401/10
    • The invention relates to compounds of formula (I), where: A is a bond, an oxygen atom, or an -CH2— group; Ar1 is a phenyl or heteroaryl group; Ar2 is a phenyl, heteroaryl, or heterocycloalkyl group; R1a,b,c and R2a,b,c are a hydrogen or halogen atom, or an alkyl, cycloalkyl, or lkyl-cycloalkyl group optionally substituted by one or more halogen atoms, or an —OR5 (hydroxy or alkoxy), hydroxy-alkyl, alkoxy-alkyl, alkoxy-alkoxy, halogenoalkyl, —O-halogenoalkyl, oxo, —CO-alkyl, —CO-alkyl-NR6R7, —CO-halogenoalkyl, —COOR5, alkyl-COOR5, —O-alkyl-COOR5, —SO2-alkyl, —SO2-cycloalkyl, —SO2-alkyl-cycloalkyl, —SO2-alkyl-OR5, —SO2-alkyl-COOR5, —SO2-alkyl-NR6R7, —SO2-halogenoalkyl, alkyl-SO2-alkyl, —SO2—NR6R7, —SO2-alkyl-O-alkyl-OR5, —CONR6R7, -alkyl-CONR6R7, or -alkyl-NR6R7 group, or further R1a, R1b, and R1c are bonded to R2a, R2b, R2c, respectively, as well as to the carbon atom having same, and are -alkyl-O—; R3 is a hydrogen atom or an alkyl group; R4 is a ONR6R7 group, a hydroxyalkyl group substituted by a halogenoalkyl group, or an lkyl-NH—SO2-alkyl, NH—SO2-alkyl, —O—SO2—NR6R7, -alkyl-CO—NR6R7, —O-alkyl-CO—NR6R7, -alkyl-NR6R7, —O—CO—NR6R7, -alkyl-heteroaryl, a heteroaryl group optionally substituted by an alkyl, alkoxy-imino, or —NH—NH—CO-alkyl group, with the proviso that R4 is in the cis position when it is the ONR6R7 group and that R6 and R7 are each hydrogen, or an lkyl or lkyl-phenyl group; R5 is hydrogen, an lkyl group, or lkyl-phenyl; R6 and R7, identical or different, are each a hydrogen atom, an alkyl group, alkoxy, or an alkyl-phenyl group; and R8 is a hydrogen atom or an O2-alkyl group, or a group of formula -Het, where B can be absent or be a bond, an oxygen atom, or a O— or O2—(CH2)n group, with n being equal to 0, 1, or 2, and where Het is a heteroaryl or heterocycloaryl optionally substituted by the alkyl, —SO2-alkyl, and —COOR5 groups. The invention also relates to a method for preparing same to the therapeutic use thereof.
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